Laboratório de Tecnologia Farmacêutica Prof. Delby Fernandes de Medeiros, Universidade Federal da Paraíba, João Pessoa, Paraíba, Brazil.
Nat Prod Res. 2012;26(24):2335-9. doi: 10.1080/14786419.2011.653974. Epub 2012 Jan 31.
We aimed to investigate the possible spasmolytic activity of ent-7α-acetoxytrachyloban-18-oic acid (1) and ent-7α-hydroxytrachyloban-18-oic acid (2) on smooth muscle models. In male rat aorta and rat uterus, both diterpenes were unable to trigger spasmolytic action. However, 2 relaxed guinea-pig trachea: Compounds 1 and 2 antagonised, significantly and concentration-dependently, carbachol- and histamine-induced phasic contractions in guinea-pig ileum. Moreover, they induced a significant and concentration-dependent relaxation in pre-contracted (KCl, carbachol or histamine) guinea-pig ileum, with 2 being 15 times more potent than 1 in histamine-contracted ileum. These dissimilar results may be due to chemical differences between them. Thus, we demonstrated that 1 and 2 seem to be promising spasmolytic agents, although further studies are required to elucidate the spasmolytic action mechanism.
我们旨在研究 ent-7α-乙酰氧基千里光菲烷-18-酸(1)和 ent-7α-羟基千里光菲烷-18-酸(2)对平滑肌模型可能的松弛作用。在雄性大鼠主动脉和大鼠子宫中,这两种二萜均不能引发松弛作用。然而,化合物 2 松弛了豚鼠气管:化合物 1 和 2 显著且浓度依赖性地拮抗了在豚鼠回肠中引起的由卡巴胆碱和组胺引起的阵发性收缩。此外,它们在预收缩(KCl、卡巴胆碱或组胺)的豚鼠回肠中引起了显著且浓度依赖性的松弛,在组胺收缩的回肠中,2 的作用比 1 强 15 倍。这些不同的结果可能是由于它们之间的化学差异所致。因此,我们证明 1 和 2 似乎是有前途的松弛剂,尽管需要进一步研究来阐明其松弛作用机制。